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Activators and Inhibitors of Protein Kinase C (PKC): Their Applications in Clinical Trials

Protein kinase C (PKC), a family of phospholipid-dependent serine/threonine kinase, is classed into three subfamilies based on their structural and activation characteristics: conventional or classic PKC isozymes (cPKCs; α, βI, βII, and γ), novel or non-classic PKC isozymes (nPKCs; δ, ε, η, and θ),...

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Autores principales: Kawano, Takahito, Inokuchi, Junichi, Eto, Masatoshi, Murata, Masaharu, Kang, Jeong-Hun
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2021
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8621927/
https://www.ncbi.nlm.nih.gov/pubmed/34834162
http://dx.doi.org/10.3390/pharmaceutics13111748
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author Kawano, Takahito
Inokuchi, Junichi
Eto, Masatoshi
Murata, Masaharu
Kang, Jeong-Hun
author_facet Kawano, Takahito
Inokuchi, Junichi
Eto, Masatoshi
Murata, Masaharu
Kang, Jeong-Hun
author_sort Kawano, Takahito
collection PubMed
description Protein kinase C (PKC), a family of phospholipid-dependent serine/threonine kinase, is classed into three subfamilies based on their structural and activation characteristics: conventional or classic PKC isozymes (cPKCs; α, βI, βII, and γ), novel or non-classic PKC isozymes (nPKCs; δ, ε, η, and θ), and atypical PKC isozymes (aPKCs; ζ, ι, and λ). PKC inhibitors and activators are used to understand PKC-mediated intracellular signaling pathways and for the diagnosis and treatment of various PKC-associated diseases, such as cancers, neurological diseases, cardiovascular diseases, and infections. Many clinical trials of PKC inhibitors in cancers showed no significant clinical benefits, meaning that there is a limitation to design a cancer therapeutic strategy targeting PKC alone. This review will focus on the activators and inhibitors of PKC and their applications in clinical trials.
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spelling pubmed-86219272021-11-27 Activators and Inhibitors of Protein Kinase C (PKC): Their Applications in Clinical Trials Kawano, Takahito Inokuchi, Junichi Eto, Masatoshi Murata, Masaharu Kang, Jeong-Hun Pharmaceutics Review Protein kinase C (PKC), a family of phospholipid-dependent serine/threonine kinase, is classed into three subfamilies based on their structural and activation characteristics: conventional or classic PKC isozymes (cPKCs; α, βI, βII, and γ), novel or non-classic PKC isozymes (nPKCs; δ, ε, η, and θ), and atypical PKC isozymes (aPKCs; ζ, ι, and λ). PKC inhibitors and activators are used to understand PKC-mediated intracellular signaling pathways and for the diagnosis and treatment of various PKC-associated diseases, such as cancers, neurological diseases, cardiovascular diseases, and infections. Many clinical trials of PKC inhibitors in cancers showed no significant clinical benefits, meaning that there is a limitation to design a cancer therapeutic strategy targeting PKC alone. This review will focus on the activators and inhibitors of PKC and their applications in clinical trials. MDPI 2021-10-20 /pmc/articles/PMC8621927/ /pubmed/34834162 http://dx.doi.org/10.3390/pharmaceutics13111748 Text en © 2021 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Review
Kawano, Takahito
Inokuchi, Junichi
Eto, Masatoshi
Murata, Masaharu
Kang, Jeong-Hun
Activators and Inhibitors of Protein Kinase C (PKC): Their Applications in Clinical Trials
title Activators and Inhibitors of Protein Kinase C (PKC): Their Applications in Clinical Trials
title_full Activators and Inhibitors of Protein Kinase C (PKC): Their Applications in Clinical Trials
title_fullStr Activators and Inhibitors of Protein Kinase C (PKC): Their Applications in Clinical Trials
title_full_unstemmed Activators and Inhibitors of Protein Kinase C (PKC): Their Applications in Clinical Trials
title_short Activators and Inhibitors of Protein Kinase C (PKC): Their Applications in Clinical Trials
title_sort activators and inhibitors of protein kinase c (pkc): their applications in clinical trials
topic Review
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8621927/
https://www.ncbi.nlm.nih.gov/pubmed/34834162
http://dx.doi.org/10.3390/pharmaceutics13111748
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